Molecules,
Journal Year:
2024,
Volume and Issue:
29(9), P. 2127 - 2127
Published: May 3, 2024
Neurodegeneration
is
a
gradual
decay
process
leading
to
the
depletion
of
neurons
in
both
central
and
peripheral
nervous
systems,
ultimately
resulting
cognitive
dysfunctions
deterioration
brain
functions,
alongside
decline
motor
skills
behavioral
capabilities.
Neurodegenerative
disorders
(NDs)
impose
substantial
socio-economic
strain
on
society,
aggravated
by
advancing
age
world
population
absence
effective
remedies,
predicting
negative
future.
In
this
context,
urgency
discovering
viable
therapies
critical
and,
despite
significant
efforts
medicinal
chemists
developing
potential
drug
candidates
exploring
various
small
molecules
as
therapeutics,
regrettably,
truly
treatment
yet
be
found.
Nitrogen
heterocyclic
compounds,
particularly
those
containing
indole
nucleus,
which
has
emerged
privileged
scaffold,
have
attracted
particular
attention
for
variety
pharmacological
applications.
This
review
analyzes
rational
design
strategy
adopted
different
research
groups
development
anti-neurodegenerative
indole-based
compounds
modulate
molecular
targets
involved
NDs,
with
reference
most
recent
advances
between
2018
2023.
Journal of Medicinal Chemistry,
Journal Year:
2022,
Volume and Issue:
65(13), P. 8550 - 8595
Published: June 27, 2022
A
person
suspected
of
having
Alzheimer's
disease
(AD)
is
clinically
diagnosed
for
the
presence
principal
biomarkers,
especially
misfolded
amyloid-beta
(Aβ)
and
tau
proteins
in
brain
regions.
Existing
radiotracer
diagnostic
tools,
such
as
PET
imaging,
are
expensive
have
limited
availability
primary
patient
screening
pre-clinical
animal
studies.
To
change
status
quo,
small-molecular
near-infrared
(NIR)
probes
been
rapidly
developed,
which
may
serve
an
inexpensive,
handy
imaging
tool
to
comprehend
dynamics
pathogenic
progression
AD
assess
therapeutic
efficacy
vivo.
This
Perspective
summarizes
biochemistry
Aβ
then
focuses
on
structurally
diverse
NIR
with
coverages
their
spectroscopic
properties,
binding
affinity
toward
species,
theranostic
effectiveness.
With
summarized
information
perspective
discussions,
we
hope
that
this
paper
a
guiding
designing
novel
vivo
fluoroprobes
capabilities
future.
Journal of Enzyme Inhibition and Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
38(1)
Published: Feb. 20, 2023
Alzheimer's
disease
(AD),
a
persistent
neurological
dysfunction,
has
an
increasing
prevalence
with
the
aging
of
world
and
seriously
threatens
health
elderly.
Although
there
is
currently
no
effective
treatment
for
AD,
researchers
have
not
given
up,
are
committed
to
exploring
pathogenesis
AD
possible
therapeutic
drugs.
Natural
products
attracted
considerable
attention
owing
their
unique
advantages.
One
molecule
can
interact
multiple
AD-related
targets,
thus
having
potential
be
developed
in
multi-target
drug.
In
addition,
they
amenable
structural
modifications
increase
interaction
decrease
toxicity.
Therefore,
natural
derivatives
that
ameliorate
pathological
changes
should
intensively
extensively
studied.
This
review
mainly
presents
research
on
AD.
Phytomedicine Plus,
Journal Year:
2023,
Volume and Issue:
3(2), P. 100439 - 100439
Published: March 30, 2023
Alzheimer's
disease
(AD)
is
a
neurodegenerative
with
cognitive
and
memory
decline.
Due
to
the
lack
of
effective
treatment
for
AD,
there
an
interest
in
finding
novel
compounds
treat
AD.
The
leaves
Adhatoda
vasica
Nees
(AV)
exhibited
anti-AD
effects
known
be
rich
pyrroloquinazoline
alkaloids.
However,
role
alkaloids
as
was
not
explored.
Therefore,
present
study
aimed
isolate
active
through
bioactivity
guided
fractionation
from
AV
explore
their
effect.
Column
chromatography
dichloromethane
(DCM)
fraction
methanolic
extract
used
AV.
isolated
were
characterized
by
TLC,
HPLC,
ATR,
HRMS,
NMR
techniques.
In-silico,
studies
performed
investigate
interaction
cholinesterase
enzymes
(AChE
BuChE).
Further,
in-vitro
assays
carried
out
evaluate
AChE,
BuChE,
Aβ
inhibition
properties.
Propidium
iodide
displacement
assay
know
selectivity
at
AChE
PAS
site.
Furthermore,
in-vivo
improvement
against
scopolamine-induced
amnesia
induced
neurotoxicity
rats.
A
couple
leads
identified
fractionation,
such
vasicinone
(VAS)
vasicine
(VA)
responsible
DCM
fraction.
In-silico
that
both
stable
interactions
BuChE
sites.
VAS
VA
inhibited
aggregation
effectively
displaced
propidium
showed
administration
significantly
improved
dysfunction
scopolamine
impairments
Besides,
recovered
hippocampal
cell
density
AD
Moreover,
did
show
any
sign
toxicity.
revealed
acts
potent
agent
it
similar
potency
profile
impairment
Both
possess
strong
potential
preclinical
development
natural
drugs
anti-AD.
Drug Development Research,
Journal Year:
2023,
Volume and Issue:
84(8), P. 1624 - 1651
Published: Sept. 11, 2023
Alzheimer's
disease
(AD)
is
a
progressive
age-related
neurodegenerative
brain
disorder,
which
leads
to
loss
of
memory
and
other
cognitive
dysfunction.
The
underlying
mechanisms
AD
pathogenesis
are
very
complex
still
not
fully
explored.
Cholinergic
neuronal
loss,
accumulation
amyloid
plaque,
metal
ions
dyshomeostasis,
tau
hyperphosphorylation,
oxidative
stress,
neuroinflammation,
mitochondrial
dysfunction
major
hallmarks
AD.
current
treatment
options
for
acetylcholinesterase
inhibitors
(donepezil,
rivastigmine,
galantamine)
NMDA
receptor
antagonists
(memantine).
These
FDA-approved
drugs
mainly
provide
symptomatic
relief
without
addressing
the
pathological
aspects
progression.
So,
there
an
urgent
need
novel
drug
development
that
only
addresses
basic
but
also
shows
neuroprotective
property.
Various
research
groups
across
globe
working
on
multifunctional
agents
amelioration
using
different
core
scaffolds
their
design,
carbamate
among
them.
Rivastigmine
was
first
investigated
management.
fragment,
scaffold
act
as
potential
inhibitor
acetylcholinesterase.
In
this
review,
we
summarize
last
10
years
conducted
modification
with
substituents
primarily
target
ChE
inhibition,
reduce
modulate
Aβ
aggregation.
